US5153005A - Composition and method for preventing fluorosis - Google Patents

Composition and method for preventing fluorosis Download PDF

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Publication number
US5153005A
US5153005A US07/625,563 US62556390A US5153005A US 5153005 A US5153005 A US 5153005A US 62556390 A US62556390 A US 62556390A US 5153005 A US5153005 A US 5153005A
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US
United States
Prior art keywords
fluoride
monofluorophosphate
ingestible
sodium
fluorosis
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
US07/625,563
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English (en)
Inventor
Marcus G. Grodberg
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Colgate Palmolive Co
Original Assignee
Colgate Palmolive Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Colgate Palmolive Co filed Critical Colgate Palmolive Co
Priority to US07/625,563 priority Critical patent/US5153005A/en
Priority to ZA919577A priority patent/ZA919577B/xx
Priority to MX9102376A priority patent/MX9102376A/es
Priority to EP19910311437 priority patent/EP0494512A3/en
Priority to IE426491A priority patent/IE914264A1/en
Priority to PT99725A priority patent/PT99725A/pt
Priority to FI915801A priority patent/FI915801A/fi
Priority to CA002057336A priority patent/CA2057336A1/en
Priority to GR910100499A priority patent/GR1001380B/el
Priority to AU89632/91A priority patent/AU651402B2/en
Priority to JP3327705A priority patent/JPH04287660A/ja
Priority to BR919105340A priority patent/BR9105340A/pt
Assigned to COLGATE-PALMOLIVE COMPANY reassignment COLGATE-PALMOLIVE COMPANY ASSIGNMENT OF ASSIGNORS INTEREST. Assignors: GRODBERG, MARCUS G.
Application granted granted Critical
Publication of US5153005A publication Critical patent/US5153005A/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/42Phosphorus; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis

Definitions

  • This invention relates to a fluorosis-free ingestible fluoride ion-containing composition useful as a dietary supplement for use alone or as an additive to milk, baby formula or other beverages or foods for users of all ages, particularly infants and young children.
  • the fluorosis-free composition of the present invention is distinct from non-ingested oral treatment compositions containing binary fluoride sources of sodium fluoride and sodium monofluorophosphate such as are described in U.S. Pat. Nos. 4,152,419, 4,425,324 and 4,528,181, as well as British Patent No. 1 435 624.
  • a combination of a pharmaceutically acceptable fluoride such as sodium fluoride (NaF) and a monofluorophosphate, such as a sodium monofluorophosphate (MFP) provides an ingestible composition for fluorosis-free anticaries treatment which is uniquely compatible with dietary products, and particularly calcium-containing foods, such as milk.
  • a pharmaceutically acceptable fluoride such as sodium fluoride (NaF)
  • a monofluorophosphate such as a sodium monofluorophosphate (MFP)
  • MFP sodium monofluorophosphate
  • Sodium monofluorophosphate is known to be slowly metabolized by an intestinal enzyme, alkaline phosphatase, converting monofluorophosphate into free fluoride ion which, in turn, is absorbed into the bloodstream.
  • the invention is applicable to the alkali metal, ammonium and amine cations, the preferred by far, is the sodium salt.
  • sodium fluoride where the fluoride ion is immediately available as such, the available fluoride constitutes 45% by weight of the amount of sodium fluoride present; with sodium monofluorophosphate (MFP) the potential available fluoride constitutes 13% of the weight of the compound.
  • MFP sodium monofluorophosphate
  • the amount of fluoride ion from sodium fluoride is about three and one half times the potential amount from an equal weight of monofluorophosphate; therefore, at a weight ratio of monofluorophosphate to NaF of 3.5:1, we have about fifty percent of the total fluoride ion from NaF and fifty percent from monofluorophosphate.
  • MFP/NaF weight ratio
  • a weight ratio of MFP to NaF of about 10.5:1 we have twenty-five percent of the fluoride ion from NaF and seventy-five percent from MFP.
  • monofluorophosphate e.g. sodium MFP
  • sodium fluoride combinations are compatible with vitamin-mineral pharmaceutical compositions, such as used in pre- and post-natal dietary supplements.
  • Ingestible drops preferably aqueous, which can be added to milk, formula for infants, and like beverages, form an ideal vehicle for providing a desired dosage for infants and up to teenagers while aiding in the prevention of fluorosis. It is convenient to prepare such compositions so that they provide from about 0.05 to about 0.38 mg of total fluoride ion per drop, whereby a few drops can provide from about 0.25 mg fluoride which is the total recommended dosage for infants to 1.0 mg, the recommended dosage from three years of age to the teens.
  • An aqueous composition is prepared combining 800 mg of MFP and 70 mg of sodium fluoride dissolved in sufficient water to make 100 ml of solution.
  • This solution contains 1.36 mg F-/ml (1.04 mg from MFP and 0.32 from NaF).
  • the composition contains 0.076 mg F-/drop.
  • the aforedescribed prescriptions of fluoride salt and monofluorophosphate may further be defined in terms of percent by weight of each.
  • the foregoing tablet is formulated to provide about one milligram of fluoride ion which is suitable for use by older children (three years and up), adults and pre-natal women.

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
US07/625,563 1990-12-11 1990-12-11 Composition and method for preventing fluorosis Expired - Fee Related US5153005A (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
US07/625,563 US5153005A (en) 1990-12-11 1990-12-11 Composition and method for preventing fluorosis
ZA919577A ZA919577B (en) 1990-12-11 1991-12-04 Composition and method for preventing fluorosis
MX9102376A MX9102376A (es) 1990-12-11 1991-12-04 Composicion y metodo para evitar la fluorosis.
IE426491A IE914264A1 (en) 1990-12-11 1991-12-09 Composition and method for preventing fluorosis
PT99725A PT99725A (pt) 1990-12-11 1991-12-09 Processo para a preparacao de uma composicao ingerivel contendo iao fluoreto para inibicao de fluorose
EP19910311437 EP0494512A3 (en) 1990-12-11 1991-12-09 Composition and method for preventing fluorosis
FI915801A FI915801A (fi) 1990-12-11 1991-12-10 Komposition och foerfarande foer att foerhindra fluoros.
CA002057336A CA2057336A1 (en) 1990-12-11 1991-12-10 Composition and method for preventing fluorosis
GR910100499A GR1001380B (el) 1990-12-11 1991-12-11 Σύν?εση και μέ?οδος για πρόληψη φ?όρωσης.
AU89632/91A AU651402B2 (en) 1990-12-11 1991-12-11 Composition and method for preventing fluorosis
JP3327705A JPH04287660A (ja) 1990-12-11 1991-12-11 フッ素症を予防する組成物とその方法
BR919105340A BR9105340A (pt) 1990-12-11 1991-12-11 Composicao ingerivel contendo ion fluoreto isenta de fluorose e aperfeicoamento em um processo para evitar ou minimizar a formacao de manchas nos dentes de criancas

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/625,563 US5153005A (en) 1990-12-11 1990-12-11 Composition and method for preventing fluorosis

Publications (1)

Publication Number Publication Date
US5153005A true US5153005A (en) 1992-10-06

Family

ID=24506665

Family Applications (1)

Application Number Title Priority Date Filing Date
US07/625,563 Expired - Fee Related US5153005A (en) 1990-12-11 1990-12-11 Composition and method for preventing fluorosis

Country Status (12)

Country Link
US (1) US5153005A (es)
EP (1) EP0494512A3 (es)
JP (1) JPH04287660A (es)
AU (1) AU651402B2 (es)
BR (1) BR9105340A (es)
CA (1) CA2057336A1 (es)
FI (1) FI915801A (es)
GR (1) GR1001380B (es)
IE (1) IE914264A1 (es)
MX (1) MX9102376A (es)
PT (1) PT99725A (es)
ZA (1) ZA919577B (es)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030157145A1 (en) * 2002-01-24 2003-08-21 Kalili Tom K. Fluoridated products
US20040101493A1 (en) * 2002-11-26 2004-05-27 Scott Douglas Craig Chewable solid unit dosage forms and methods for delivery of active agents into occlusal surfaces of teeth
US20040101494A1 (en) * 2002-11-26 2004-05-27 Scott Douglas Craig Chewable solid unit dosage forms and methods for delivery of active agents into occlusal surfaces of teeth
US8911805B2 (en) 2010-03-31 2014-12-16 Toyo Suisan Kaisha, Ltd. Calcium preparation and method of production thereof

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5683678A (en) * 1995-03-09 1997-11-04 The Procter & Gamble Company Oral compositions
FR2857827B1 (fr) * 2003-07-25 2006-02-24 United Pharmaceuticals Sa Nouveaux produits alimentaires titres en fluor et leur utilisation pour assurer un developpement dentaire et osseux harmonieux
FR2857826A1 (fr) * 2003-07-25 2005-01-28 United Pharmaceuticals Sa Procede pour charger les aliments en fluor et leur utilisation pour assurer un developpement osseux harmonieux

Citations (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1013756A (fr) * 1950-02-14 1952-08-04 Produit alimentaire
BE731578A (es) * 1969-04-16 1969-10-01
GB1221633A (en) * 1968-01-16 1971-02-03 Sten Yngve Ericsson Compositions for hardening teeth and bones
GB1249852A (en) * 1967-08-06 1971-10-13 William John Bendall Improvements relating to the treatment of milk
FR2239205A1 (en) * 1973-08-02 1975-02-28 Biotherapie Drinkable fluorinated milk in concentrate or powder form - as nourishment with anti-caries activity for the young
US4083955A (en) * 1975-04-02 1978-04-11 The Procter & Gamble Company Processes and compositions for remineralization of dental enamel
US4169885A (en) * 1977-03-19 1979-10-02 Blendax-Werke R. Schneider Gmbh & Co. Dental and oral hygiene preparations
US4397837A (en) * 1972-02-02 1983-08-09 Blendax-Werke R. Schneider Gmbh & Co. Process and composition for the remineralization and prevention of demineralization of animal teeth including humans
US4424203A (en) * 1983-03-04 1984-01-03 Pakhomov Gennady N Gel for dental caries prevention
US4460565A (en) * 1981-07-03 1984-07-17 Intradal N.V. Anticariogenic remineralizing dentifrice
US4556561A (en) * 1983-03-25 1985-12-03 American Dental Association Health Foundation Compositions and methods for topically fluoridating and/or mineralizing dental tissue
US4627978A (en) * 1984-12-21 1986-12-09 Ici Americas Inc. Tooth drop dentifrice formulation and method of treating teeth, mouth and throat therewith to reduce plaque accumulation and irritation
US4693888A (en) * 1983-08-11 1987-09-15 Lion Corporation Caries-preventive composition
US4726952A (en) * 1983-08-11 1988-02-23 Mission Pharmacal Slow-release sodium fluoride tablet, method of making, and method of treatment of osteoporosis
US4728513A (en) * 1985-07-31 1988-03-01 Zyma Sa Granular delayed-release form of pharmaceutically active substances
CA1237082A (en) * 1982-12-29 1988-05-24 Johannes F. Laimbock Foodstuffs
US4784858A (en) * 1985-08-29 1988-11-15 Zyma Sa Controlled release tablet
US4859467A (en) * 1986-09-25 1989-08-22 Colgate-Palmotive Company Sustained release fluoride composition
US4861590A (en) * 1986-09-25 1989-08-29 Colgate-Palmolive Company Sustained release fluoride and calcium composition
US4904478A (en) * 1983-08-11 1990-02-27 Mission Pharmacal Company Slow-release sodium fluoride tablet and method for treatment of osteoporosis
US4915948A (en) * 1987-08-31 1990-04-10 Warner-Lambert Company Tablets having improved bioadhesion to mucous membranes
US5013728A (en) * 1990-05-04 1991-05-07 Colgate - Palmolive Company Composition for treating osteoporosis and hormonal imbalance

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4152419A (en) * 1977-05-25 1979-05-01 Colgate-Palmolive Company Dentifrice composition

Patent Citations (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1013756A (fr) * 1950-02-14 1952-08-04 Produit alimentaire
GB1249852A (en) * 1967-08-06 1971-10-13 William John Bendall Improvements relating to the treatment of milk
GB1221633A (en) * 1968-01-16 1971-02-03 Sten Yngve Ericsson Compositions for hardening teeth and bones
BE731578A (es) * 1969-04-16 1969-10-01
US4397837A (en) * 1972-02-02 1983-08-09 Blendax-Werke R. Schneider Gmbh & Co. Process and composition for the remineralization and prevention of demineralization of animal teeth including humans
FR2239205A1 (en) * 1973-08-02 1975-02-28 Biotherapie Drinkable fluorinated milk in concentrate or powder form - as nourishment with anti-caries activity for the young
US4083955A (en) * 1975-04-02 1978-04-11 The Procter & Gamble Company Processes and compositions for remineralization of dental enamel
US4169885A (en) * 1977-03-19 1979-10-02 Blendax-Werke R. Schneider Gmbh & Co. Dental and oral hygiene preparations
US4460565A (en) * 1981-07-03 1984-07-17 Intradal N.V. Anticariogenic remineralizing dentifrice
CA1237082A (en) * 1982-12-29 1988-05-24 Johannes F. Laimbock Foodstuffs
US4424203A (en) * 1983-03-04 1984-01-03 Pakhomov Gennady N Gel for dental caries prevention
US4556561A (en) * 1983-03-25 1985-12-03 American Dental Association Health Foundation Compositions and methods for topically fluoridating and/or mineralizing dental tissue
US4693888A (en) * 1983-08-11 1987-09-15 Lion Corporation Caries-preventive composition
US4726952A (en) * 1983-08-11 1988-02-23 Mission Pharmacal Slow-release sodium fluoride tablet, method of making, and method of treatment of osteoporosis
US4904478A (en) * 1983-08-11 1990-02-27 Mission Pharmacal Company Slow-release sodium fluoride tablet and method for treatment of osteoporosis
US4627978A (en) * 1984-12-21 1986-12-09 Ici Americas Inc. Tooth drop dentifrice formulation and method of treating teeth, mouth and throat therewith to reduce plaque accumulation and irritation
US4728513A (en) * 1985-07-31 1988-03-01 Zyma Sa Granular delayed-release form of pharmaceutically active substances
US4784858A (en) * 1985-08-29 1988-11-15 Zyma Sa Controlled release tablet
US4859467A (en) * 1986-09-25 1989-08-22 Colgate-Palmotive Company Sustained release fluoride composition
US4861590A (en) * 1986-09-25 1989-08-29 Colgate-Palmolive Company Sustained release fluoride and calcium composition
US4915948A (en) * 1987-08-31 1990-04-10 Warner-Lambert Company Tablets having improved bioadhesion to mucous membranes
US5013728A (en) * 1990-05-04 1991-05-07 Colgate - Palmolive Company Composition for treating osteoporosis and hormonal imbalance

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
Biotherapie C.A. 83:183398s (1985) of Fr. Dem. 2,239,205. *
Ericsson C.A. 73:38547d (1970) of Belg. 731,578. *
Fuchs et al C.A. 91:186370c (1979). *
Ruzicka et al C.A. 82:1188799 (1974). *
Skobe et al C.A. 103:135128p (1985). *
Trautner et al C.A. 110:128095s (1989). *
Trautner et al C.A. 111:83977h (1989). *
Villa et al C.A. 110:2304885 (1989). *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030157145A1 (en) * 2002-01-24 2003-08-21 Kalili Tom K. Fluoridated products
US20040101493A1 (en) * 2002-11-26 2004-05-27 Scott Douglas Craig Chewable solid unit dosage forms and methods for delivery of active agents into occlusal surfaces of teeth
US20040101494A1 (en) * 2002-11-26 2004-05-27 Scott Douglas Craig Chewable solid unit dosage forms and methods for delivery of active agents into occlusal surfaces of teeth
US8911805B2 (en) 2010-03-31 2014-12-16 Toyo Suisan Kaisha, Ltd. Calcium preparation and method of production thereof

Also Published As

Publication number Publication date
CA2057336A1 (en) 1992-06-12
EP0494512A2 (en) 1992-07-15
MX9102376A (es) 1993-01-01
FI915801A0 (fi) 1991-12-10
PT99725A (pt) 1992-10-30
IE914264A1 (en) 1992-06-17
BR9105340A (pt) 1992-08-25
AU8963291A (en) 1992-06-18
GR1001380B (el) 1993-10-29
FI915801A (fi) 1992-06-12
JPH04287660A (ja) 1992-10-13
AU651402B2 (en) 1994-07-21
EP0494512A3 (en) 1993-03-17
ZA919577B (en) 1993-09-06
GR910100499A (en) 1992-11-23

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